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Synonyms: eflapegrastim-xnst | HM-10460A | HM10460A | rolontis | Rolvedon® | SPI-2012 | SPI2012
eflapegrastim is an approved drug (FDA (2022))
Compound class:
Peptide or derivative
Comment: Eflapegrastim (SPI-2012) is a long-acting, human granulocyte colony-stimulating factor (G-CSF) recombinant peptide. Structurally it consists of a recombinant G-CSF (1-174) peptide monomer and an IgG4 Fc dimer, that are joined by a PEG-derived linker molecule. G-CSF stimulates neutrophil progenitor proliferation and differentiation, a molecular mechanism that is exploited to reduce the incidence and severity of chemotherapy-induced neutropenia. The Fc fragment increases the drug's half-life (reduces clearance) and overall efficacy by improving uptake into the bone marrow via binding to Fc receptors on the endothelial cells [1].
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Peptide Sequence  |
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hG-CSFmonomerTPLGPASSLPQSFLLKSLEQVRKIQGDGAALQEKLCATYKLCHPEELVLLGHSLGIPWAPLSSCSSQ ALQLAGCLSQLHSGLFLYQGLLQALEGISPELGPTLDTLQLDVADFATTIWQQMEELGMAPALQPTQGAMPAFASAFQRR AGG150VLVASHLQSFLEVSYRVLRHLAQP:hIGHG4FcmonomerPSCPAPEFLGGPSVFLFPPKPKDTLMISRTPEVT CVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAK GQPREPQVYTLPPSQEEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEG NVFSCSVMHEALHNHYTQKSLSLSLGK |
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| Chemical Modification | |
| Dimer (G-CSF-Fc) formed by monomers that are linked by a polyethylene glycol derivative. | |
